Target-oriented synthesis of antiparasitic 2-hetaryl substituted quinolines based on imino Diels-Alder reactions

被引：32
|
作者：
Kouznetsov, Vladimir V. [1 ]
Vargas Mendez, Leonor Y.
Milena Leal, Sandra
Mora Cruz, Uriel
Andres Coronado, Carlos
Melendez Gomez, Carlos M.
Romero Bohorquez, Arnold R.
Escobar Rivero, Patricia
机构：
[1] Univ Ind Santander, Escuela Quim, CIBIMOL, Lab Quim Organ & Biomol, Bucaramanga 678 AA, Colombia
[2] Univ Ind Santander, Escuela Med, Dept Ciencias Basicas, CINTROP,Ctr Invest Enfermedades Trop, Bucaramanga 678 AA, Colombia
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2007年 / 4卷 / 04期
关键词：
antiparasitic activities; target-oriented synthesis; 2-hetarylquinolines; Leishmania chagasi; trypanosoma cruzi; drug discovery;
D O I：
10.2174/157018007784620031
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Target-oriented synthesis of new substituted 2-hetarylquinolines 6-19 and their in vitro activity against endemic parasites such as Leishmania chagasi and Trypanosoma cruzi are reported. In addition, their cytotoxicities for mammalian Vero cells and THP-1 macrophages cells are assessed. These studies showed that between the new (tetrahydro)quinolines series tested in these assays, the 4-methyl-8-isopropyl-2-(3-pyridinyl)quinoline 15 exhibits the best in vitro response against both live forms of T. cruzi and L. chagasi parasites and displays no cytotoxic activity on mammalian cells.
引用
收藏
页码：293 / 296
页数：4
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